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Anastrozole
drug data and news
Anastrozole drug data, resources, and news articles (when available). Onconews.org provides news on cancer research. This section, which includes profiles on medicines that may or not be cancer-related is in beta form. If things run smoothly we will be releasing a new format late in the summer of 2006.
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| Generic name | Anastrozole | ||
| Brand Names/Synonyms | Anastrole; Anastrozol; Anastrozole; Anastrozole [Usan:Ban:Inn]; Arimidex; CHEMBANK1630; ICI-D 1033; ZD 1033 | ||
| Indication | For treatment of advanced breast cancer. | ||
| Sponsored links | Description | Not Available | |
| Pharmacology | Anastrozole is a potent and selective non-steroidal aromatase inhibitor indicated for the treatment of advanced breast cancer in post-menopausal women with disease progression following tamoxifen therapy. Many breast cancers have estrogen receptors and growth of these tumors can be stimulated by estrogens. In post-menopausal women, the principal source of circulating estrogen (primarily estradiol) is conversion of adrenally-generated androstenedione to estrone by aromatase in peripheral tissues, such as adipose tissue, with further conversion of estrone to estradiol. Many breast cancers also contain aromatase; the importance of tumor-generated estrogens is uncertain. Treatment of breast cancer has included efforts to decrease estrogen levels by ovariectomy premenopausally and by use of anti-estrogens and progestational agents both pre- and post-menopausally, and these interventions lead to decreased tumor mass or delayed progression of tumor growth in some women. Anastrozole is a potent and selective non-steroidal aromatase inhibitor. It significantly lowers serum estradiol concentrations and has no detectable effect on formation of adrenal corticosteroids or aldosterone. | ||
| Mechanism Of Action | Anastrozole selectively inhibits aromatase. The principal source of circulating estrogen (primarily estradiol) is conversion of adrenally-generated androstenedione to estrone by aromatase in peripheral tissues. Therefore, aromatase inhibition leads to a decrease in circulatin estrogen, leading to a decreased tumor mass or delayed progression of tumor growth in some women. | ||
| Anastrozole News (When available) |
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| Dosage Forms | tablets containing 1mg anastrozole | ||
| Drug_Category | Antineoplastic Agents; ATC:L02BG03 | ||
| Absorption | Absorbed into the systemic cirulation, and food does not affect the extent of absorption. | ||
| Interactions |
-->Interactions for Anastrozole: Anastrozole inhibited in vitro metabolic reactions catalyzed by cytochromes P450 1A2, 2C8/9, and 3A4 but only at relatively high concentrations. Anastrozole did not inhibit P450 2A6 or the polymorphic P450 2D6 in human liver microsomes. Anastrozole did not alter the pharmacokinetics of antipyrine. Although there have been no formal interaction studies other than with antipyrine, based on these in vivo and in vitro studies, it is unlikely that co-administration of a 1 mg dose of ARIMIDEX with other drugs will result in clinically significant drug inhibition of cytochrome P450-mediated metabolism of the other drugs. An interaction study with warfarin showed no clinically significant effect of anastrozole on warfarin pharmacokinetics or anticoagulant activity. At a median follow-up of 33 months, the combination of ARIMIDEX and tamoxifen did not demonstrate any efficacy benefit when compared with tamoxifen in all patients as well as in the hormone receptor-positive subpopulation. This treatment arm was discontinued from the trial. Based on clinical and pharmacokinetic results from the ATAC trial, tamoxifen should not be administered with anastrozole (see CLINICAL PHARMACOLOGY ñ Drug Interactions and CLINICAL PHARMACOLOGY - Clinical Studies - Adjuvant Treatment of Breast Cancer in Postmenopausal Women subsections). Co-administration of anastrozole and tamoxifen resulted in a reduction of anastrozole plasma levels by 27% compared with those achieved with anastrozole alone. Estrogen-containing therapies should not be used with ARIMIDEX as they may diminish its pharmacologic action. Drug/Laboratory Test Interactions No clinically significant changes in the results of clinical laboratory tests have been observed. --> | ||
| Toxicity | In rats, lethality is greater than 100mg/kg. | ||
| Organisms Affected | Humans and other mammals | ||
| Chemical IUPAC Name | 2-[3-(1-cyano-1-methyl-ethyl)-5-(1H-1,2,4-triazol-1-ylmethyl)phenyl]-2-methyl-propanenitrile | ||
| Chemical Formula | C17H19N5 | ||
| Molecular Weight | 293.366 g/mol | ||
| Smiles String | CC(C)(C#N)C1=CC(=CC(=C1)CN2C=NC=N2)C(C)(C)C#N | ||
| Melting Point | 130.14 °C | ||
| Water Solubility | 0.5mg/ml | ||
| State | off-white powder | ||
| LogP/Hphobicity | 4.501 | ||
| Isoelectric Point | Not Available | ||
| Biotransformation | Hepatic. Metabolized mainly by N -dealkylation, hydroxylation, and glucuronidation to inactive metabolites. Primary metabolite is an inactive triazole. | ||
| Half Life | 50 hours | ||
| Protein Binding [%] | 40% | ||
| RxList Link | RXlist | ||
| Sponsored links | |||
| Drug Reference |
http://www.drugs.com/cons/Anastrozole.html http://www.rxlist.com/cgi/generic2/anastr.htm | ||
| Drug Type | Approved Drug | ||
| Accession No | APRD00016 | ||
| CAS Registry Number | 120511-73-1 | ||
| KEGG Compound ID | C08159 | ||
| PubChem ID | SID:63297 | ||
| PharmGKB ID | PA448432 | ||
| SwissProt ID | Not Available | ||
| GenBank ID | Not Available | ||
| Drug ID Number [DIN] | 2224135 |
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